1. Field of the Invention
The invention relates to 2'-alkylsulfonylsteroido[3,2-d]thiazoles, which are useful as antiandrogenic agents, and processes for preparation, method of use and compositions thereof.
2. Information Disclosure Statement
Christiansen et al. U.S. Pat. No. 4,684,636 issued Aug. 4, 1987 describes antiandrogenic sulfonylsteroidopyrazoles including as EXAMPLE 1 the compound having the structural formula ##STR1## which showed relative binding affinities of 2.1 at 1 hr. and 0.09 at 18 hr. in the rat prostate androgen receptor competition assay and an AED.sub.50 value of 14 mg./kg. orally in the test for antiandrogenic activity in the castrated immature male rat.
Clinton U.S. Pat. No. 3,081,228 issued Mar. 12, 1963 describes 2'-amino-5.alpha.-androst-2-eno[3,2-d]thiazoles having hypotensive activity and having the structural formula ##STR2## wherein "R represents hydrogen or a lower-alkyl radical, and R' represents hydrogen or a carboxylic acyl radical."
Doorenbos et al. (Journal of Pharmaceutical Sciences, vol. 50, p. 271, 1961) describes the preparation of five 17.alpha.-methyl-5.alpha.-androst-2-eno[3,2-d]thiazole-17.beta.-ols having the following structural formula but does not describe any biological property thereof. ##STR3##
Denes et al. (Journal of the Chemical Society, Chemical Communications, sec. D, no. 11, p. 621, 1969) describes the preparation of 2'-methyl-5.alpha.-cholest-2-eno[3,2-d]thiazole and 2'-methyl-5.alpha.-androst-2-eno[3,2-d]thiazol-17.beta.-ol but does not describe any biological property thereof.